| 货号 | 11900-50mg |
| 描述 | AMP-activated protein kinase (AMPK) is an αβγ heterotrimer that functions as a metabolic sensor, regulating lipid and glucose metabolism to maintain cellular energy homeostasis and to protect against metabolic stress.1 A-769662 is a small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.2,3 A-769662 specifically activates β1 subunit-containing AMPK heterotrimers, and its effects are independent of kinases upstream of AMPK.2,4 A-769662 has been used to stimulate CYP450-mediated fatty acid oxidation, inhibit adipocyte differentiation, explore glucose uptake in skeletal muscle, and promote endothelial cell survival during metabolic stress.4,5,6,7,8 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hardie, D.G., and Carling, D. The AMP-activated protein kinase. Fuel gauge of the mammalian cell? European Journal of Biochemistry 246, 259-273 (1997). 2.Göransson, O.,McBride, A.,Hawley, S.A., et al. Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase. The Journal of Biological Chemisty 282(45), 32549-32560 (2007). 3.Sanders, M.J.,Ali, Z.S.,Hegarty, B.D., et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. The Journal of Biological Chemisty 282(45), 32540-32548 (2007). 4.Scott, J.W.,van Denderen, B.J.W.,Jorgensen, S.B., et al. Thienopyridone drugs are selective activators of AMP-activated protein kinase β1-containing complexes. Chemistry & Biology 15, 1220-1230 (2013). 5.Zhou, Y.,Wang, D.,Zhu, Q., et al. Inhibitory effects of A-769662, a novel activator of AMP-activated protein kinase, on 3T3-L1 adipogenesis. Biological and Pharmaceutical Bullentin 32(6), 993-998 (2009). 6.Hsu, M.H.,Savas, Ü.,Lasker, J.M., et al. Genistein, resveratrol, and 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside induce cytochrome P450 4F2 expression through an AMP-activated protein kinase-dependent pathway. Journal of Pharmacology and Experimental Therapeutics 337(1), 125-136 (2011). 7.Treebak, J.T.,Birk, J.B.,Hansen, B.F., et al. A-769662 activates AMPK β1-containing complexes but induces glucose uptake through a PI3-kinase-dependent pathway in mouse skeletal muscle. American Journal of Physiology.Cell Physiology 297, C1041-C1052 (2009). 8.Liu, X.m.,Peyton, K.J.,Shebib, A.R., et al. Activation of AMPK stimulates heme oxygenase-1 gene expression and human endothelial cell survival. American Journal of Physiology.Heart and Circulatory Physiology 300, H84-H93 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 360.4 |
| 分子式 | C20H12N2O3S |
| CAS号 | 844499-71-4 |
| 稳定性 | ≥ 2 years |
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